Abstract
The need for develo** new antimalarials has been expressed on various occasions by the World Health Organization (WHO). The “Special Programme for Research and Training in Tropical Diseases” (TDR), established in 1975 under the auspices of the UNDP, World Bank and WHO (1980), has stimulated new efforts in this field. The highest priority has been given to the development of new antimalarials.
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References
Ahmad RA, Rogers HJ (1981) Salivary elimination of pyrimethamine. Br J Clin Pharmacol 11:101–102
Alving AS, Coggeshall LT (1974) Clinical testing of antimalarial drugs at Stateville Penitentiary, Malaria report 30. National Institute of Health, Washington
Ambroise-Thomas P (1974) La réaction d’immunofluorescence dans l’étude séro-immuno-logique du paludisme. Bull WHO 50:267–276
Arnold JD, Martin DC, Carson PE, Rieckmann KH, Willerson D Jr, Clyde DF, Miller RM (1973) A phenanthrene methanol (WR 33063) for treatment of acute malaria. Antimicrob Agents Chemother 3:207–213
Aronsson L, Bengtsson E, Björkan A, Pehrson PO, Rombo L, Wahlgren M (1981) Chloro-quine-resistant falciparum malaria in Madagascar and Kenya. Ann Trop Med Parasitol 75:367–373
Ballif-Negulici E, Constantinesco P (1963) Therapeutic effects of a single dose of pyrimethamine in malaria inoculation with local or imported strains of P. vivax and P. falciparum. Arch Roum Pathol Exp Microbiol 22:997–1002
Berliner RW, Earle P Jr, Taggart JV et al. (1948) Studies on the chemotherapy of the human malarias VI. The physiological disposition, antimalarial activity, and toxicity of several derivatives of 4-aminoquinoline. J Clin Invest 27:98–107
Black RH, Dew BB, Hennessy WB, McMillan B, Torpy DC (1966) Studies on depot antimalarials: I. The effect of a single injection of the depot antimalarial CI-501 (Camolar) on relapsing vivax malaria acquired in New Guinea. Med J Aust 2:588–592
Blackwell B, Stolley PD, Buncher R, Klimt CR, Temple R, Venn D, Wardell WM (1975) Panel 4: Phase IV investigations. Clin Pharmacol Ther 18:653–656
Brohult J, Rombo L, Sirleaf V, Bengtsson E (1979) The concentration of chloroquine in serum during short- and long-term malaria prophylaxis with standard and “double” dosage in non-immunes: clinical implications. Ann Trop Med Parasitol 73:401–405
Bruce-Chwatt LJ (1967) Clinical trials of antimalarial drugs. Trans R Soc Trop Med Hyg 61:412–426
Canfield CJ, Hall AP, MacDonald BS, Neumann DA, Shaw JA (1973) Treatment of falciparum malaria from Vietnam with a phenanthrene methanol (WR 33063) and a quinoline methanol (WR 30090). Antimicrob Agents Chemother 3:224–227
Canfield CR, Rozman RS (1974) Clinical testing of new antimalarial compounds. Bull WHO 50:203–212
Chaput de Saintonge DM (1978) Klinische Prüfungen — leichter gesagt als getan. Internist (Berlin) 19:349–356
Chin W, Contacos PG, Coatney GR, Kimball HR (1965) A naturally acquired quotidian-type malaria in man transferable to monkeys. Science 149:865
Chin W, Rattanartihikul M (1973) The evaluation of the presumptive and radical treatments against falciparum malaria in Thailand. Southeast Asian J Trop Med Public Health 4:400–406
Clyde DF, Miller RM, DuPont HL, Hornick RB (1971) Antimalarial effects of tetracyclines in man. J Trop Med Hyg 74:238–242
Clyde DF, McCarthy VC, Miller RM, Hornick RB (1973) Specificity of protection of man immunized against sporozoite-induced falciparum malaria. Am J Med Sci 266:398–403
Clyde DF, McCarthy VC, Miller RM, Woodward WE (1975) Immunization of man against falciparum and vivax malaria by use of attenuated sporozoites. Am J Trop Med Hyg 4:397–401
Contacos PG, Coatney GR, Lunn JS, Kilpatrick JW (1964) The antimalarial activity of CI-501 (Camolar) against falciparum malaria. Am J Trop Med Hyg 13:386–390
Covell G, Coatney GR, Field JW, Singh I (1956) La chimiothérapie du paludisme. Monograph Series WHO 27:1–132
Degơin RL, Eppes RB, Carson PE, Powell RD (1966) The effects of diaphenyl-sulfone (DDS) against chloroquine-resistant Plasmodium falciparum. Bull WHO 34:671–681
Desjardins RE, Pamplin CL, Von Bredow J, Barry KG, Canfield CJ (1979) Kinetics of a new antimalarial, mefloquine. Clin Pharmacol Ther 26:372–379
Draper CC (1971) Laboratory diagnosis. Br Med J 2:93–95
Ebisawa I, Komoriya T, Kimura M, Muto T (1974) Morphological and clinical effects of pyrimethamine-sulfonamide combinations (sulformethoxine-pyrimethamine or sulfa-monomethoxine-pyrimethamine) on P. vivax and its infection. Jpn J Exp Med 44:151–163
Food and Drug Administration (1977 a) General considerations for the clinical evaluation of drugs. US Department of Health, Education and Welfare, Washington, DC
Food and Drug Administration (1977 b) Guidelines for the clinical evaluation of anti-infective drugs (systemic adults and children) US Department of Health, Education and Welfare, Washington, DC
Food and Drug Administration (1977 c) General considerations for the clinical evaluation of drugs in infants and children. US Department of Health, Education and Welfare, Washington, DC
George CF (1974) The investigation of new drugs in man. Br J Hosp Med 780–787
Gerberg EJ (1971) Evaluation of antimalarial compounds in mosquito test systems. Trans R Soc Trop Med Hyg 65:358–363
Gilles HM, Clyde DF (1974) Acetylator phenotype in sulphonamide-resistant falciparum malaria. Ann Trop Med Parasitol 68:367–368
Goldberg LI, Besselaar GH, Arnold JD, Lemberger L, Mitchell JR, Whitset TL (1975) Panel 1: Phase I investigations. Clin Pharmacol Ther 18:643–646
Grin EI, Pirnat L, Dimitrijevic E, Simic L (1973) Thromboangiitis and results obtained by pyretotherapy using malaria. Excerpta Medica, Public Health Social Medicine and Hygiene 21:1–53
Hall AP, Doberstyn EB, Nanakorn A, Sonkom A (1975 a) Falciparum malaria semi-resistant to clindamycin. Br Med J 2:12–14
Hall AP, Doberstyn EB, Mettaprakong V, Sonkom P (1975 b) Falciparum malaria cured by quinine followed by sulfadoxine-pyrimethamine. Br Med J 2:15–17
Haskins WT (1958) A simple qualitative test for chloroquine in urine. Am J Trop Med 7:199–222
Hickman RL (1969) The use of subhuman primates for experimental studies of human malaria. Milit Med 134:741–756
Jauch R, Griesser E, Oesterhelt G (1980) Metabolismus von Ro 21–5998 (Mefloquin) bei der Ratte. Arzneimittelforsch 30:60–67
Jusko WJ (1981) Smoking and drug response. Trends Pharm Int 2:10–13
Kahl GF (1978) Interaktionen von Arzneimitteln: Ein Problem bei der Therapie. Internist (Berlin) 19:366–374
Killick-Kendrick R, Peters W (1978) Rodent malaria. Academic, London, p 406
Krotoski WA, Garnham PCC, Bray RS, Krotoski DM, Killick-Kendrick R, Draper CC, Targett GAT, Guy WM (1980) The hypnozoite of Plasmodium cynomolgi: true latent stage in malarial relapse? 29 th Annual meeting. Am Soc Trop Med Hyg, Atlanta
Lasagna L (1975) Clinical trials of drugs from the viewpoint of the academic investigator (a satire). Clin Pharmacol Ther 18:629–633
Lasagna L (1979) The diseases and drug needs of the Third World. J Chronic Dis 32:413–414
Liss RL, Kensler CJ (1976) Advances in modern toxicology. In: Mehlman MA, Shapiro RE, Blumenthal H (eds) New concepts in safety evaluation. Hemisphere, Washington, DC, p273
Lupascu G (1974) Applications actuelles de la malaria thérapie. Bull WHO 50:165–168
Mannweiler E, Mohr W, Felde I zum, Hinrichs A, Haas J (1976) Zur Serodiagnostik der Malaria. MMW 118:1139–1144
Merkli B, Richie R (1980) Studies on the resistance to single and combined antimalarials in the Plasmodium berghei mouse model. Acta Trop (Basel) 37:228–231
Merkli B, Richie R, Peters W (1980) The inhibitory effect of a drug combination on the development of mefloquine resistance in Plasmodium berghei. Ann Trop Med Parasitol 74:1–9
Meuwissen JHET, Leeuwenberg ADEM, Voller A, Matola Y (1974) Specificity of the indirect haemagglutination test with Plasmodium falciparum test cells. Bull WHO 50:513–519
Miller LH, Glew RH, Wyler DJ, Howard WA, Collins WE, Contacos PG, Neva FA (1974) Evaluation of clindamycin in combination with quinine against multidrug-resistant strains of Plasmodium falciparum. Am J Trop Med Hyg 23:565–569
Mu JY, Iraili ZH, Dayton PG (1975) Studies of the disposition and metabolism of mefloquine HCl (WR 142490), a quinoline-methanol antimalarial, in the rat. Drug Metab Dispos 3:198–210
Peters W (1970) Chemotherapy and drug resistance in malaria. Academic, New York
Peters W (1979) 4- and 8-Aminoquinoline, Chinin und Chinin-ähnliche Verbindungen. Hahnenklee Symposium Roche Grenzach, BRD
Picq JJ, Charmot G, Ricosse JH (1972) A comparative study between a single dose of py-rimethamine-sulfamethopyrazine compound and a single dose of chloroquine for the treatment of acute attack of P. falciparum malaria in “semi-immune” subjects living in an endemic area (Bobo-Dioulasso, Upper Volta). Méd Trop 32:527–546
Powell RD, Brewer GJ (1967) Effects of pyrimethamine, chlorguanide, and primaquine against exoerythrocytic forms of a strain of chloroquine-resistant Plasmodium falciparum from Thailand. Am J Trop Med Hyg 16:693–698
Rawlins MD (1974) Variability of response to drugs in man. Br J Hosp Med 803–811
Rieckmann KH (1971) Determination of the drug sensitivity of Plasmodium falciparum. JAMA 217:573–578
Rieckmann KH, McNamara JV, Frischer H, Stockert TA, Carson PE, Powell RD (1968) Effects of chloroquine, quinine, and cycloguanil upon the maturation of asexual erythrocytic forms of two strains of Plasmodium falciparum in vitro. Am J Trop Med Hyg 17:661–671
Rieckmann KH, Trenholme GM, Williams RL, Carson PE, Frischer H, Desjardins RE (1974) Prophylactic activity of mefloquine hydrochloride (WR 142490) in drug-resistant malaria. Bull WHO 51:375–377
Rieder J (1976) The simultaneous quantitative determination of total, “active,” acetylated and conjugated sulfonamide in biological fluids. Chemotherapy 22:84–87
Rozman RS, Molek NA, Koby R (1978) The absorption, distribution, and excretion in mice of the antimalarial mefloquine, erythro-2,8-bis(trifluoromethyl)-α-(2-piperidyl)-4-quinoline-methanol hydrochloride. Drug Metab Dispos 6:654–658
Schwartz DE (1980) Quantitative determination of the antimalarial drug mefloquine and of its main metabolite in plasma by direct densitometric measurement on TLC plates. In: Frigerio, McCamish (eds) Recent developments in chromatography and electrophoresis, vol 10. Elsevier, Amsterdam, pp 69–74
Schwartz DE, Weber W, Richard-Lenoble D, Gentillini M (1980) Kinetic studies of mefloquine and one of its metabolites, Ro 21–5104, in the dog and in man. Acta Trop (Basel) 37:238–242
Schwartz DE, Eckert G, Hartmann D, Weber B, Richard-Lenoble D, Ekue JMK, Gentilini M (1982) Single-dose kinetics of mefloquine in man. Plasma levels of the unchanged drug and of one of its metabolites. Chemotherapy 28:70–84
Smith CC, Weigel WW, Wolfe GF (1973) Excretion and tissue localization patterns of experimental antimalarial agents. Fed Proc 32:701
Staiger MA, Nguyen-Dinh P, Churchill C (1981) Sensitive high-performance liquid chromatographic analysis for chloroquine in body fluids. Application to studies of drug resistance in Plasmodium falciparum. J Chromatogr 225:139–149
Trenholme GM, Williams RL, Desjardins RE, Frischer H, Carson PE, Rieckmann KH, Canfield CJ (1975) Mefloquine (WR 142490) in the treatment of human malaria. Science 190:792–794
Ungureanu E, Killick-Kendrick R, Garnham PCC, Branzei P, Romanescu C, Shute PG (1976) Prepatent periods of a tropical strain of Plasmodium vivax after inoculations of tenfold dilutions of sporozoites. Trans R Soc Trop Med Hyg 70:482–483
Wernsdorfer WH (1980) Field evaluation of drug resistance in malaria. In vitro micro-test. Acta Trop (Basel) 37:222–227
WHO (1961) Chemotherapy of malaria. WHO Tech Rep Ser 226
WHO (1968) WHO expert committee on malaria. 14 th Report. Tech Rep Ser 382
WHO (1973) Chemotherapy of malaria and resistance to antimalarials. WHO Tech Rep Ser 529
WHO (1974) Symposium on Malaria Research. Bull WHO 50:1–372
WHO (1975 a) Developments in malaria immunology. WHO Tech Rep Ser 579
WHO (1975 b) Guidelines for evaluation of drugs for use in man. WHO Tech Rep Ser 563
WHO (1977) USAID/WHO Workshops on the biology and in vitro cultivation of malaria parasites. Bull WHO 55, n. 2–3:121–429
WHO (1979) Instruction for the use of the WHO Test Kit for the assessment of the response of Plasmodium falciparum to chloroquine. WHO Document MAP/79.1
WHO (1980) The clinical management of acute malaria. WHO Reg Publ SE Asia Ser 9
Wilson M, Fife EH Jr, Methews HM, Sulzer AJ (1975) Comparison of the complement fixation, indirect immunofluorescence, and indirect hemagglutination tests for malaria. Am J Trop Med Hyg 24:755–759
Wiselogle FY (1946) A survey of antimalarial drugs 1941–1945. Edwards, Ann Arbor
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Fernex, M. (1984). Clinical Trials — Phases I and II. In: Peters, W., Richards, W.H.G. (eds) Antimalarial Drugs I. Handbook of Experimental Pharmacology, vol 68 / 1. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-69251-2_13
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DOI: https://doi.org/10.1007/978-3-642-69251-2_13
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